Assay Detail
Functional
CHEMBL4701868
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Agonist activity at human KOR stably expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by liquid scintillation counting assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 6.36 | 7.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4761165 | — | — | 1 | 7.33 |
| CHEMBL4776986 | — | — | 1 | 6.80 |
| CHEMBL4749016 | — | — | 1 | 6.62 |
| CHEMBL4742666 | — | — | 1 | 6.40 |
| CHEMBL4747286 | — | — | 1 | 6.40 |
| CHEMBL4798887 | — | — | 1 | 6.38 |
| CHEMBL4745899 | — | — | 1 | 6.37 |
| CHEMBL4789659 | — | — | 1 | 6.29 |
| CHEMBL4750783 | — | — | 1 | 5.81 |
| CHEMBL4758754 | — | — | 1 | 5.80 |
| CHEMBL4744531 | — | — | 1 | 5.78 |
| CHEMBL3408737 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4761165 | — | EC50 | = | 47.1 | nM | 7.33 |
| CHEMBL4776986 | — | EC50 | = | 158.0 | nM | 6.80 |
| CHEMBL4749016 | — | EC50 | = | 239.0 | nM | 6.62 |
| CHEMBL4742666 | — | EC50 | = | 399.0 | nM | 6.40 |
| CHEMBL4747286 | — | EC50 | = | 401.0 | nM | 6.40 |
| CHEMBL4798887 | — | EC50 | = | 415.0 | nM | 6.38 |
| CHEMBL4745899 | — | EC50 | = | 424.0 | nM | 6.37 |
| CHEMBL4789659 | — | EC50 | = | 514.0 | nM | 6.29 |
| CHEMBL4750783 | — | EC50 | = | 1556.0 | nM | 5.81 |
| CHEMBL4758754 | — | EC50 | = | 1574.0 | nM | 5.80 |
| CHEMBL4744531 | — | EC50 | = | 1649.0 | nM | 5.78 |
| CHEMBL3408737 | — | EC50 | > | 10000.0 | nM | - |